Prednisolone-d7 is intended for use as an internal standard for the quantification of prednisolone by GC- or LC-MS. Prednisolone is a glucocorticoid and mineralocorticoid receptor agonist and an active metabolite of the prodrugs and synthetic glucocorticoids prednisolone phosphate and prednisone .1,2,3 It selectively binds to the glucocorticoid and mineralocorticoid receptors over the progesterone, androgen, and estrogen receptors (Kis = 2.4, 37, >5,000, 2,762, and >1,000 nM, respectively) and induces transactivation in reporter assays using CV-1 cells expressing the human glucocorticoid receptor or human mineralocorticoid receptor (EC50s = 6.9 and 3.78 nM, respectively).2,3 Prednisolone reduces pulmonary eosinophil infiltration in a rat model of sephadex-induced asthma (ED50 = 1.2 mg/kg).[2] Formulations containing prednisolone have been used as anti-inflammatory or immunosuppressive agents.
References:
[1].Frey, B.M., Seeberger, M., and Frey, F.J.Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejectionTransplantation39(3)270-274(1985).
[2].Coghlan, M.J., Kym, P.R., Elmore, S.W., et al.Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: Selective quinoline derivatives with prednisolone-equivalent functional activityJ. Med. Chem.44(18)2879-2885(2001).
[3].Grossmann, C., Scholz, T., Rochel, M., et al.Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: A comparison of their glucocorticoid and mineralocorticoid propertiesEur. J. Endocrinol.151(3)397-406(2004).